• Given the overexpression of HO in some tumors such as

  2022-03-30

  

  Given the overexpression of HO-1 in some tumors, such as CML, and its potential involvement in chemoresistance to classical chemotherapeutic agents, compounds 4 and 8f were tested in CML cell lines resistant to IM, a classical TK inhibitor used in CML. Compounds 4 and 8f, in combination with IM, sho

• We also examined possible involvement of the NF B

  2022-03-29

  

  We also examined possible involvement of the NF-κB signaling pathway in GSK-3 inhibitor-induced suppression of PGE2 production, whereas GSK-3 inhibitors did not have a significant effect on IκB phosphorylation/degradation or NF-κB nuclear translocation. These results are consistent with a previous p

• Hypoxia has been shown to affect

  2022-03-29

  

  Hypoxia has been shown to affect miR-155 expression that can induce autophagy in nasopharyngeal and cervical carcinoma cells [334]. Suppression of miR-155 inhibited hypoxia-induced autophagy. miR-155 targeted mRNAs involved in the PI3K/PTEN/Akt/mTORC1 pathway including: Ras homolog enriched in m1 re

• In addition researchers studying GPR agonists favor the

  2022-03-29

  

  In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it GZD824 is unclear why Sanofi-Aventis chose to terminate collaboration with Metabolex (no

• br Materials and methods br Results br Discussion

  2022-03-29

  

  Materials and methods Results Discussion Since 1990s, solving structures for most DNA glycosylases by X-ray crystallography significantly advanced mechanistic understanding of the catalytic activity and substrate specificity of this important class of DNA repair enzymes. However, static str

• br Materials and methods br Results

  2022-03-29

  

  Materials and methods Results Discussion In nerve terminals, Na+-dependent glutamate transporters of the plasma membrane are responsible for the maintenance of low (non-toxic) extracellular glutamate concentrations and accomplish uptake of glutamate into the CD 1530 of neurons and glial ce

• In this study we present the

  2022-03-29

  

  In this study, we present the synthesis and structure–activity studies of a structurally distinct series possessing high potency and selectivity in HEK cell lines together with a potentially promising overall biopharmacological profile. Focusing on creating sufficient structural dissimilarity with g

• Human Glucocorticoid Receptor hGR was first cloned

  2022-03-29

  

  Human Glucocorticoid Receptor (hGR) was first cloned in 1985 (Hollenburg et al., 1985). It is a modular protein comprised of an N-terminal trans-activating domain (NTD), a C-terminal ligand-binding domain (LBD) and a central DNA- binding domain (DBD). The DBD is highly conserved and has two zinc fin

• Considerable evidence links sustained GCG administration

  2022-03-29

  

  Considerable evidence links sustained GCG administration to the reduction of food intake, enhancement of energy expenditure and weight loss in rodent and human studies [16], [17], [18]. Moreover, patients presenting with GCG-producing tumors frequently manifest severe weight loss, through mechanisms

• Extensive pharmacological and structural analysis shows GCGR

  2022-03-29

  

  Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in ikk inhibitor 14, 17, 20. Functionally identical to REMD-477, REMD2

• In summary our findings provide the evidence

  2022-03-29

  

  In summary, our findings provide the evidence and the mechanistic understanding of the protective effects of GIP receptor agonist, D-Ala2GIP, in the MPTP-induced neurotoxicity in mice. The observed protective effects are potentially due to reduced oxidative stress and attenuation of dopamine loss in

• In this study we demonstrate that the ETS

  2022-03-29

  

  In this study, we demonstrate that the ETS transcription factor ETV5 is involved in the regulation of ghrelin system in response to the altered nutritional state. In the recent multiple GWAS studies, three single nucleotide polymorphisms (SNPs) of ETV5, rs7647305 (Thorleifsson et al., 2009; Willer e

• br Acknowledgements We apologize to our distinguished collea

  2022-03-29

  

  Acknowledgements We apologize to our distinguished colleagues whose work has not been cited owing to space limitations. This work was funded by the Italian Association for Cancer Research (AIRC, Milan, Italy, IG 14732 to A.M.); Italian Ministry of University and Education (Finanziamenti per la Ri

• Ligand selectivity may directly be related to the conformati

  2022-03-29

  

  Ligand selectivity may directly be related to the conformational landscape explored by GPCRs despite that most GPCRs do not require dimerization for ligand recognition (Mary et al., 2012). Monomer FPRs have traditionally been perceived as receptors that can recognize N-formyl peptides and LXA4. This

• Sensitivity to EphB TKI was also demonstrated in a colon

  2022-03-29

  

  Sensitivity to EphB3 TKI was also demonstrated in a colon cancer cell line, COLO 205, with high expression of EphB3. We found not only exogenous but also endogenous EphB3 protein was expressed in the COLO 205 tsa inhibitor after transient transfection of pCMV6-AC-GFP/EphB3, and both were demonstrat

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